NCT05555823

Safety, Tolerability, Pharmacokinetics, Pharmacodynamics, Food Effect and DDI of Ascending Doses of the MEK Inhibitor Zapnometinib

A Phase I Dose Escalation Study of Ascending Single and Multiple Doses of the MEK Inhibitor Zapnometinib in Healthy Subjects to Evaluate the Safety & Tolerability Compared to Placebo, Additionally Evaluating Pharmacokinetics and Pharmacodynamics of Target Engagement, as Well as Investigating Possible FDI and DDI

• Status: Completed
• Phase: Phase 1
• Study type: Interventional
• Enrollment: 96 (actual)
• Sponsor: Atriva Therapeutics GmbH · Industry
• Sex: All
• Age: 18 Years – 55 Years
• Healthy volunteers: Accepted

Summary

The purpose of this study is to evaluate the safety and tolerability of ascending doses of the MEK-inhibitor zapnometinib (ATR-002) given as single doses (SAD Part) and as multiple doses for 7 days (MAD Part) in healthy subjects.

Detailed description

This is a Phase 1, single-center, randomized, double-blind, controlled clinical trial (zapnometinib vs. placebo in the SAD/MAD Parts; 'fed' vs. 'fasted' in the FDI Part, 'probe substance' (repaglinide or celecoxib) in combination with zapnometinib vs. probe substance alone in the DDI part). The study will assess the safety, tolerability, PK (applicable to SAD/MAD Part) and PD (applicable to SAD Part only) effects of zapnometinib versus a matching placebo (applicable to SAD/MAD Part) in healthy subjects. The FDI cohorts will investigate the possible impact of a standard breakfast high in fat content in comparison to administration in fasted state. The DDI cohorts with celecoxib and repaglinide will investigate a possible drug-drug interaction.

Conditions

• Healthy

Interventions

Type	Name	Description
DRUG	ATR-002	300 mg tablets for oral intake
DRUG	Placebo	matching tablets for oral intake
DRUG	Repaglinide	0,5 mg tablets for oral intake
DRUG	Celecoxib	100 mg capsules for oral intake

Timeline

• Start date: 2022-06-23
• Primary completion: 2023-07-20
• Completion: 2023-07-20
• First posted: 2022-09-27
• Last updated: 2023-08-01

Locations

1 site across 1 country: Germany